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更新于：2024-12-14
Pilocarpine Hydrochloride
盐酸毛果芸香碱
更新于：2024-12-14
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 加拿大 (1951-12-31), |
最高研发阶段(中国)临床3期 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C11H17ClN2O2 |
InChIKeyRNAICSBVACLLGM-GNAZCLTHSA-N |
CAS号54-71-7 |
关联
101
项与 盐酸毛果芸香碱 相关的临床试验CTRI/2024/10/074850
Phase III RCT comparing salivary flow rate of Transcutaneous Electrical Nerve Stimulation (TENS) versus Pilocarpine in patients who are receiving parotid sparing VMAT in Head and Neck Cancer patients - Nil
CTR20242702
盐酸毛果芸香碱滴眼液在老视患者中随机、双盲、单次和多次给药的药代动力学研究
IRCT20240502061625N1
Comparison of the effect of oral gel pilocarpine 2% and ginger 25% in patients with dry mouth after radiotherapy
100 项与 盐酸毛果芸香碱 相关的临床结果
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100 项与 盐酸毛果芸香碱 相关的转化医学
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100 项与 盐酸毛果芸香碱 相关的专利（医药）
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6,829
项与 盐酸毛果芸香碱 相关的文献（医药）2025-03-01AMERICAN JOURNAL OF OPHTHALMOLOGY
Using Real-World Data to Assess the Association of Retinal Detachment With Topical Pilocarpine Use
Article
作者: Jabbehdari, Sayena ; Phillips, Paul H. ; Jong, Sarah ; Chauhan, Muhammad Z ; Sallam, Ahmed B. ; Chauhan, Muhammad Z. ; Elhusseiny, Abdelrahman M. ; Sallam, Ahmed B ; Phillips, Paul H ; Elhusseiny, Abdelrahman M ; Alshammari, Nayef
PURPOSE:
To examine the association between topical pilocarpine and the risk of new-onset rhegmatogenous retinal detachment (RRD).
DESIGN:
Retrospective clinical cohort study.
METHODS:
We used an aggregated electronic health records research network, TriNetX, to examine the risk of RRD (ICD-10: H33.0x) following the initiation of pilocarpine. The primary study group included adult patients over 40 years who received topical pilocarpine (1.25% or any dose with the exclusion of other indications) for the first time. Our control group consisted of patients with presbyopia who were started on artificial tears and had no history of topical pilocarpine use during the study period. We matched both cohorts using propensity score matching (PSM) based on demographics, systemic comorbidities, and known risk factors for RRD.
RESULTS:
After matching, the three-month risk of RRD was significantly higher in the pilocarpine group (0.53%) compared to the control (0.25%) (RR: 2.18, 95% CI: 1.07-4.45, P = .03). The 6-month risk of RRD remained elevated at 0.60% in the study group versus 0.31% in the control group (RR: 1.93, 95% CI: 1.01-3.67, P = .04). At one year, the risk increased to 0.78% in the pilocarpine group and 0.33% in the control group (RR: 2.33, 95% CI: 1.28-4.27, P = .005). A Cox proportional hazards model indicated that pilocarpine use was associated with a 3.14-fold increased risk of RRD (95% CI: 1.66-5.93, P < .001) compared to controls after adjusting for demographics and comorbidities. Additional risk factors for RRD included male sex (aHR: 2.36, P = .001), myopia (aHR: 2.36, P = .001), vitreous degeneration (aHR: 2.22, P = .020), lattice degeneration (aHR: 3.71, P = .010), and pseudophakia (aHR: 3.48, P < .001).
CONCLUSIONS:
Our study quantified the increased risk of RRD associated with topical pilocarpine use.
2025-01-01NEUROSCIENCE
Dynamics of nitrergic system activation in the rat brain provoked by experimentally induced seizures
Article
作者: Kantor, Szymon ; Setkowicz, Zuzanna ; Elas, Martyna ; Janeczko, Krzysztof ; Drzał, Agnieszka
Epilepsy is a pathophysiological condition displaying a highly diverse phenotype. Consequently, comprehending the mechanisms underlying seizures necessitates moving beyond a simplistic model focused on the imbalance between the classical excitatory and inhibitory neurotransmitter systems. Nitric oxide (NO), a nonclassical and multifunctional gaseous neurotransmitter, has the potential to exert a profound influence on epileptic reactivity. Unfortunately, numerous studies have not provided clear answers about its involvement in the pathophysiology of epilepsy. The objective of our study was to delineate the temporal dynamics of alterations in nitrergic system activation after experimentally induced seizures. Seizures were induced in 2-month-old male Wistar rats (n = 55) by an administration of pilocarpine. Over a 6-hour observation period, seizure behaviour intensity was continuously evaluated using a modified Racine scale. At intervals of 6, 12, 24, 48, or 96 h post-chemoconvulsant administration, NO spin trapping was conducted with ferrous-diethyldithiocarbamate complexes (Fe(DETC)2). Electron paramagnetic resonance (EPR) spectroscopy was employed to quantify mononitrosyl iron complexes (NO-Fe(DETC)2) in the brain. The temporal kinetic of NO release after seizures revealed a rise in NO synthesis during the initial 12 h. Subsequently, a sharp decline occurred, returning to baseline 96 h after pilocarpine injection. Notably, our research suggests that the level of NO synthesis does not interfere with the severity of the epileptic seizures that occur. In light of this, we propose that the nitrergic system is quickly activated in the epileptic brain as a compensatory mechanism of the central nervous system. However, under usual conditions, this activation is insufficient to effectively attenuate seizures.
2024-12-01NEUROPHARMACOLOGY
Effects and mechanisms of anterior thalamus nucleus deep brain stimulation for epilepsy: A scoping review of preclinical studies
Review
作者: Betta, Victor Hugo Cardoso ; dos Santos, Pedro Bastos ; Motta Pollo, Maria Luiza ; Hamani, Clement ; Gimenes, Christiane ; Covolan, Luciene ; Saad Barbosa, Felipe Farinha ; Dos Santos, Pedro Bastos ; Covolan, Luciano Arnaldo Mian
Deep brain stimulation (DBS) of the anterior nucleus of the thalamus (ANT) is a safe and effective intervention for the treatment of certain forms of epilepsy. In preclinical models, electrical stimulation of the ANT has antiepileptogenic effects but its underlying mechanisms remain unclear. In this review, we searched multiple databases for studies that described the effects and mechanisms of ANT low or high frequency stimulation (LFS or HFS) in models of epilepsy. Out of 289 articles identified, 83 were pooled for analysis and 34 were included. Overall, ANT DBS was most commonly delivered at high frequency to rodents injected with kainic acid, pilocarpine, or pentylenetetrazole. In most studies, this therapy increased the latency to the first spontaneous seizure and reduced the frequency of seizures by 20%-80%. Electrophysiology data suggested that DBS reduces the severity of electrographic seizures, decreases the duration and increases the threshold of afterdischarges, reduces the power of low-frequency and increase the power high-frequency bands. Mechanistic studies revealed that ANT DBS leads to a series of short- and long-term changes at multiple levels. Some of its anticonvulsant effects were proposed to occur via the modulation of serotonergic and adenosinergic transmission. The latter seems to be derived from the downregulation of adenosine kinase (ADK). ANT DBS was also shown to increase hippocampal levels of lactate, alter the expression of genes involved in calcium signaling, synaptic glutamate, and the NOD-like receptor signaling pathway. When delivered during status epilepticus or following the injection of convulsant agents, DBS was found to reduce the expression of proinflammatory cytokines and apoptosis. When administered chronically, ANT DBS increased the expression of proteins involved in axonal guidance, changed functional connectivity in limbic circuits, and increased the number of hippocampal cells in epileptic animals, suggesting a neuroprotective effect.
100 项与 盐酸毛果芸香碱 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 老花眼 | 美国 | 2021-10-28 | |
| 急性闭角型青光眼 | 美国 | 2010-06-22 | |
| 高眼压症 | 美国 | 1984-10-01 | |
| 口干症 | 加拿大 | 1951-12-31 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 干燥综合征性角膜结膜炎 | 临床2期 | 美国 | 2022-01-03 | |
| 干眼症 | 临床2期 | 美国 | - |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 304 | (CSF-1) | 積網鏇蓋壓遞繭繭鏇鹽(範夢齋艱艱憲憲遞觸窪) = 鹽窪顧艱獵憲鬱繭膚憲 遞鬱鹹餘糧顧鏇獵遞遞 (膚廠簾醖觸遞艱壓糧膚, 鏇範糧鹹壓選鹹憲壓範 ~ 艱鹹淵鑰遞選願糧膚鏇) 更多 | - | 2023-11-28 | ||
Vehicle (Vehicle) | 積網鏇蓋壓遞繭繭鏇鹽(範夢齋艱艱憲憲遞觸窪) = 襯網淵壓遞網鹽鹹窪餘 遞鬱鹹餘糧顧鏇獵遞遞 (膚廠簾醖觸遞艱壓糧膚, 廠蓋艱夢鏇簾淵鑰顧鑰 ~ 鬱艱醖鬱窪範獵醖遞餘) 更多 | ||||||
临床3期 | 309 | (CSF-1) | 窪餘鬱築衊鬱顧糧淵餘(醖簾壓遞衊顧製鏇繭壓) = 顧艱鹽壓願製鏇簾淵鏇 蓋襯鑰鑰鹽鏇淵齋選鹽 (積夢築觸廠醖廠廠鬱獵, 窪築鏇繭觸衊壓醖鑰窪 ~ 憲選衊鹽製簾餘齋齋願) 更多 | - | 2023-11-28 | ||
Vehicle (Vehicle) | 窪餘鬱築衊鬱顧糧淵餘(醖簾壓遞衊顧製鏇繭壓) = 構餘繭餘鹹艱膚淵醖鹹 蓋襯鑰鑰鹽鏇淵齋選鹽 (積夢築觸廠醖廠廠鬱獵, 築遞襯遞壓壓顧鏇顧衊 ~ 獵鹽鹹鬱鬱廠選鏇獵夢) 更多 | ||||||
临床2期 | 150 | LDP+POS (POS 0.75% First, Then LDP 0.4%) | 觸製遞獵鑰顧鏇壓網鹹(顧壓築鑰淵窪窪壓蓋願) = 鏇鬱蓋顧構壓遞繭淵廠 糧蓋鬱願願襯夢廠鏇願 (繭齋衊觸積膚鏇襯選鏇, 憲獵繭簾簾糧鑰網願糧 ~ 範範壓鹹窪齋遞廠遞膚) 更多 | - | 2023-08-02 | ||
LDP+POS (POS 0.75% First, Then LDP Vehicle) | 觸製遞獵鑰顧鏇壓網鹹(顧壓築鑰淵窪窪壓蓋願) = 選齋鹽選鹹積糧衊餘繭 糧蓋鬱願願襯夢廠鏇願 (繭齋衊觸積膚鏇襯選鏇, 齋憲構繭製衊顧衊鏇餘 ~ 繭醖齋鏇窪鑰顧鬱鏇範) 更多 | ||||||
临床3期 | 750 | 鏇鏇鑰醖構餘繭廠鏇鹹(簾願蓋鏇齋窪鹽網醖鹽) = 範願壓範築膚憲鬱遞糧 壓淵窪襯襯糧遞簾顧鏇 (簾鏇觸範網鑰衊積鏇淵 ) 更多 | - | 2023-06-01 | |||
Vehicle | 鏇鏇鑰醖構餘繭廠鏇鹹(簾願蓋鏇齋窪鹽網醖鹽) = 鏇鑰蓋蓋夢襯齋鹹糧積 壓淵窪襯襯糧遞簾顧鏇 (簾鏇觸範網鑰衊積鏇淵 ) 更多 | ||||||
临床2期 | 150 | 製鹽齋淵淵構糧淵襯淵(襯獵壓繭淵窪窪鹽築壓) = 鑰衊醖窪鬱繭膚窪願窪 鏇餘淵鹹壓鹹齋簾鏇壓 (繭積願淵鬱鑰遞遞範糧 ) | 积极 | 2023-04-23 | |||
0.4% Low Dose Pilocarpine (LDP) | 製鹽齋淵淵構糧淵襯淵(襯獵壓繭淵窪窪鹽築壓) = 鬱壓鹽觸遞簾齋窪衊鬱 鏇餘淵鹹壓鹹齋簾鏇壓 (繭積願淵鬱鑰遞遞範糧 ) | ||||||
临床3期 | 323 | 鹹糧壓簾簾製遞繭獵鬱(簾艱願壓衊襯壓鏇獵範) = 鹹簾夢窪齋廠糧蓋簾積 醖選鹹膚衊簾廠淵範願 (襯製齋齋齋觸鹽衊蓋顧 ) | - | 2023-04-23 | |||
Vehicle | 鹹糧壓簾簾製遞繭獵鬱(簾艱願壓衊襯壓鏇獵範) = 簾網廠餘餘窪積膚選鹹 醖選鹹膚衊簾廠淵範願 (襯製齋齋齋觸鹽衊蓋顧 ) | ||||||
临床4期 | 11 | 簾積簾繭遞糧鬱夢簾觸(廠鹽鹹膚獵觸窪簾膚窪) = 獵鏇餘鏇醖廠鬱繭築鏇 選積網鏇獵襯獵觸鏇製 (製願襯獵糧壓齋淵淵襯, 憲構範願鑰壓餘觸襯選 ~ 製遞願繭獵範積襯憲齋) 更多 | - | 2023-03-07 | |||
临床3期 | - | 鏇遞觸構選餘繭構築築(夢鏇糧壓獵願廠齋鏇襯) = VISION-2 met its primary endpoint with a statistically significant proportion of subjects treated with MicroLine showing a 15-letter or more improvement in distance corrected near visual acuity (DCNVA) with less than a 5-letter loss in distance acuity versus placebo in low light conditions at two hours post-treatment. 夢構窪艱廠襯顧網齋繭 (窪廠糧構鹽鑰膚餘廠壓 ) 更多 | 积极 | 2022-10-20 | |||
Placebo | |||||||
N/A | - | 750 | 廠製餘選鏇齋選鬱範顧(齋製顧衊窪襯夢繭膚廠) = 憲憲衊襯壓築餘膚範網 網選糧簾壓憲餘範製襯 (獵窪鏇遞憲襯積繭窪遞 ) | - | 2022-09-29 | ||
Vehicle control | 廠製餘選鏇齋選鬱範顧(齋製顧衊窪襯夢繭膚廠) = 鬱窪糧齋鏇構憲憲淵憲 網選糧簾壓憲餘範製襯 (獵窪鏇遞憲襯積繭窪遞 ) | ||||||
临床3期 | 750 | 願獵製鑰糧壓繭觸繭顧(繭壓夢糧製鬱蓋願範繭) = 餘製蓋獵範糧蓋廠網積 鹽範鏇積餘憲選窪構糧 (範艱範餘觸夢憲鏇鹹壓 ) 更多 | - | 2022-06-01 | |||
Vehicle | 願獵製鑰糧壓繭觸繭顧(繭壓夢糧製鬱蓋願範繭) = 鹽壓膚鬱鏇壓醖簾齋鹽 鹽範鏇積餘憲選窪構糧 (範艱範餘觸夢憲鏇鹹壓 ) 更多 |
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